HUP0401984A2 - A 4. tipusú foszfodiészteráz enzim aktivitását gátló inhibitorok alkalmazása gyógyszerkészítmények előállítására és más hatóanyagokkal alkotott kombinációik - Google Patents
A 4. tipusú foszfodiészteráz enzim aktivitását gátló inhibitorok alkalmazása gyógyszerkészítmények előállítására és más hatóanyagokkal alkotott kombinációikInfo
- Publication number
- HUP0401984A2 HUP0401984A2 HU0401984A HUP0401984A HUP0401984A2 HU P0401984 A2 HUP0401984 A2 HU P0401984A2 HU 0401984 A HU0401984 A HU 0401984A HU P0401984 A HUP0401984 A HU P0401984A HU P0401984 A2 HUP0401984 A2 HU P0401984A2
- Authority
- HU
- Hungary
- Prior art keywords
- atom
- group
- inhibitors
- atoms
- mean
- Prior art date
Links
- 239000004480 active ingredient Substances 0.000 title abstract 2
- 229940082638 cardiac stimulant phosphodiesterase inhibitors Drugs 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000002571 phosphodiesterase inhibitor Substances 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 5
- 229910052799 carbon Inorganic materials 0.000 abstract 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 abstract 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 abstract 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 1
- 101100296720 Dictyostelium discoideum Pde4 gene Proteins 0.000 abstract 1
- 108010044467 Isoenzymes Proteins 0.000 abstract 1
- 102000004861 Phosphoric Diester Hydrolases Human genes 0.000 abstract 1
- 108090001050 Phosphoric Diester Hydrolases Proteins 0.000 abstract 1
- 101100082610 Plasmodium falciparum (isolate 3D7) PDEdelta gene Proteins 0.000 abstract 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 1
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical group C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 210000003979 eosinophil Anatomy 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 210000005260 human cell Anatomy 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- -1 methylenedioxy group Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
Classifications
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
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Abstract
A találmány a 4. típusú foszfodiészteráz enzim aktivitását gátlóinhibitorok (PDE IV inhibitorok) gyógyszerek előállítását célzóalkalmazására és a PDE IV inhibitorok más hatóanyagokkal alkotottkombinációira vonatkozik. A találmány többek között az (I) általánosképletű vegyületeknek és azok sztereoizomereinek, továbbá fiziológiaiszempontból elfogadható sóinak és szolvátjainak olyan gyógyszerekelőállítását célzó alkalmazására vonatkozik, amelyekkel kezelni lehetaz olyan betegeket, akiknek a betegsége vagy kóros állapotaösszefüggésben van a PDE4-izoenzimnek azzal a szerepével, amelyet azeozinnal megfesthető emberi sejtek (humán eozinofilek) aktiválódásánakés degranulálódásának a szabályozásában játszik. Az (I) általánosképletben B jelentése nitrogénatomon vagy szénatomon keresztülkapcsolódó, 1-4 nitrogén-, oxigén- és/vagy kénatomot tartalmazó,helyettesítetlen vagy halogénatommal, A-val és/vagy OA-val mono-, di-vagy triszubsztituált aromás heterociklusos csoport, amelybenzolgyűrűvel vagy piridingyűrűvel kondenzált is lehet; Q nincs jelenvagy 1-6 szénatomos alkiléncsoportot jelent; X jelentése CH2, S vagyO; R1 és R2 jelentése - egymástól függetlenül - hidrogénatom vagy A;R3 és R4 jelentése - egymástól függetlenül - -OH, OR5, -S-R5, -SO-R5,-SO2-R5, Hal, metilén-dioxi-csoport, -NO2, -NH2, -NHR5 vagy -NR5R6; R5és R6 jelentése - egymástól függetlenül - A, 3-7 szénatomoscikloalkilcsoport, 4-8 szénatomos metilén-cikloalkil-csoport vagy 2-8szénatomos alkenilcsoport; A jelentése 1-10 szénatomos alkilcsoport,amely 1-5 fluoratommal és/vagy klóratommal helyettesítve lehet; és Haljelentése fluoratom, klóratom, brómatom vagy jódatom; Ó
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP01125394 | 2001-10-31 | ||
PCT/EP2002/009596 WO2003037349A1 (en) | 2001-10-31 | 2002-08-28 | Type 4 phosphodiesterase inhibitors and uses thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0401984A2 true HUP0401984A2 (hu) | 2005-02-28 |
HUP0401984A3 HUP0401984A3 (en) | 2005-06-28 |
Family
ID=8179073
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0401984A HUP0401984A3 (en) | 2001-10-31 | 2002-08-28 | Use of type 4 phosphodiesterase inhibitors for preparation of pharmaceutical compositions and combination with other active ingredients |
Country Status (12)
Country | Link |
---|---|
US (1) | US20040259863A1 (hu) |
EP (1) | EP1463509A1 (hu) |
JP (1) | JP2005515975A (hu) |
CN (1) | CN1578665A (hu) |
AR (1) | AR037743A1 (hu) |
CA (1) | CA2462525A1 (hu) |
CZ (1) | CZ2004516A3 (hu) |
HU (1) | HUP0401984A3 (hu) |
MX (1) | MXPA04003668A (hu) |
NO (1) | NO20042229L (hu) |
SK (1) | SK1862004A3 (hu) |
WO (1) | WO2003037349A1 (hu) |
Families Citing this family (41)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7851486B2 (en) | 2002-10-17 | 2010-12-14 | Decode Genetics Ehf. | Susceptibility gene for myocardial infarction, stroke, and PAOD; methods of treatment |
US7507531B2 (en) | 2002-10-17 | 2009-03-24 | Decode Genetics Chf. | Use of 5-lipoxygenase activating protein (FLAP) gene to assess susceptibility for myocardial infarction |
JP2006516548A (ja) | 2002-12-30 | 2006-07-06 | アンジオテック インターナショナル アクツィエン ゲゼルシャフト | 迅速ゲル化ポリマー組成物からの薬物送達法 |
US20040265323A1 (en) * | 2003-05-16 | 2004-12-30 | Mccormick Beth A. | Compositions comprising pathogen elicited epithelial chemoattractant (eicosanoid hepoxilin A3), inhibitors thereof and methods of use thereof |
US20050142104A1 (en) * | 2003-11-06 | 2005-06-30 | Zeldis Jerome B. | Methods of using and compositions comprising PDE4 modulators for the treatment and management of asbestos-related diseases and disorders |
AR049384A1 (es) * | 2004-05-24 | 2006-07-26 | Glaxo Group Ltd | Derivados de purina |
GB0514809D0 (en) | 2005-07-19 | 2005-08-24 | Glaxo Group Ltd | Compounds |
EP2218442A1 (en) * | 2005-11-09 | 2010-08-18 | CombinatoRx, Inc. | Methods, compositions, and kits for the treatment of ophthalmic disorders |
DE102005055354A1 (de) * | 2005-11-21 | 2007-10-31 | Merck Patent Gmbh | Substituierte 5-Phenyl-3,6-dihydro-2-oxo-6H-[1,3,4]thiadiazine |
DE102005055355A1 (de) * | 2005-11-21 | 2007-10-31 | Merck Patent Gmbh | 3,6-Dihydro-2-oxo-6H-[1,3,4]thiadiazinderivate |
GB0524103D0 (en) * | 2005-11-26 | 2006-01-04 | Medical Res Council | Healing |
DE102005057924A1 (de) * | 2005-12-05 | 2007-06-06 | Merck Patent Gmbh | Pyridazinonderivate |
TWI436761B (zh) * | 2006-06-19 | 2014-05-11 | Otsuka Pharma Co Ltd | 使用噻唑衍生物之方法 |
DE102006037478A1 (de) | 2006-08-10 | 2008-02-14 | Merck Patent Gmbh | 2-(Heterocyclylbenzyl)-pyridazinonderivate |
DE102007025718A1 (de) * | 2007-06-01 | 2008-12-04 | Merck Patent Gmbh | Pyridazinonderivate |
DE102007025717A1 (de) * | 2007-06-01 | 2008-12-11 | Merck Patent Gmbh | Arylether-pyridazinonderivate |
DE102007026341A1 (de) | 2007-06-06 | 2008-12-11 | Merck Patent Gmbh | Benzoxazolonderivate |
DE102007032507A1 (de) | 2007-07-12 | 2009-04-02 | Merck Patent Gmbh | Pyridazinonderivate |
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DE102008037790A1 (de) * | 2008-08-14 | 2010-02-18 | Merck Patent Gmbh | Bicyclische Triazolderivate |
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JP6713982B2 (ja) | 2014-07-24 | 2020-06-24 | ファイザー・インク | ピラゾロピリミジン化合物 |
KR102061952B1 (ko) | 2014-08-06 | 2020-01-02 | 화이자 인코포레이티드 | 이미다조피리다진 화합물 |
RU2597764C2 (ru) * | 2014-12-16 | 2016-09-20 | Федеральное государственное автономное образовательное учреждение высшего образования "Уральский федеральный университет имени первого Президента России Б.Н. Ельцина" | Применение соединений класса 1,3,4-тиадиазина в качестве средства коррекции экспериментального аллоксанового сахарного диабета |
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DE4134893A1 (de) * | 1991-10-23 | 1993-04-29 | Merck Patent Gmbh | Thiadiazinone |
DE4310699A1 (de) * | 1993-04-01 | 1994-10-06 | Merck Patent Gmbh | Thiadiazinone |
DE19502699A1 (de) * | 1995-01-28 | 1996-08-01 | Merck Patent Gmbh | Arylalkyl-thiadiazinone |
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DE19533975A1 (de) * | 1995-09-14 | 1997-03-20 | Merck Patent Gmbh | Arylalkyl-diazinone |
DE19604388A1 (de) * | 1996-02-07 | 1997-08-14 | Merck Patent Gmbh | Arylalkyl-diazinone |
DE19632549A1 (de) * | 1996-08-13 | 1998-02-19 | Merck Patent Gmbh | Arylalkanoylpyridazine |
CN1273628A (zh) * | 1997-08-11 | 2000-11-15 | 株式会社荏原制作所 | 成渣燃烧处理可燃物的方法 |
DE19826841A1 (de) * | 1998-06-16 | 1999-12-23 | Merck Patent Gmbh | Arylalkanoylpyridazine |
DE19915365A1 (de) * | 1999-04-06 | 2000-10-12 | Merck Patent Gmbh | Tetrahydropyridazin-Derivate |
DE19932315A1 (de) * | 1999-07-10 | 2001-01-11 | Merck Patent Gmbh | Benzoylpyridazine |
AR029189A1 (es) * | 1999-11-02 | 2003-06-18 | Smithkline Beecham Corp | Uso de un inhibidor de fosfodiesterasa 4 y un corticoesteroide antiinflamatorio en forma combinada, separadamente o separadamente secuencial para la preparacion de un medicamento |
HUP0300689A3 (en) * | 2000-02-08 | 2003-09-29 | Smithkline Beecham Corp | Method and compositions for treating an inflammatory disease |
-
2002
- 2002-08-28 SK SK186-2004A patent/SK1862004A3/sk unknown
- 2002-08-28 MX MXPA04003668A patent/MXPA04003668A/es unknown
- 2002-08-28 US US10/494,379 patent/US20040259863A1/en not_active Abandoned
- 2002-08-28 CN CNA02821711XA patent/CN1578665A/zh active Pending
- 2002-08-28 CA CA002462525A patent/CA2462525A1/en not_active Abandoned
- 2002-08-28 HU HU0401984A patent/HUP0401984A3/hu unknown
- 2002-08-28 WO PCT/EP2002/009596 patent/WO2003037349A1/en not_active Application Discontinuation
- 2002-08-28 EP EP02802281A patent/EP1463509A1/en not_active Withdrawn
- 2002-08-28 JP JP2003539692A patent/JP2005515975A/ja active Pending
- 2002-08-28 CZ CZ2004516A patent/CZ2004516A3/cs unknown
- 2002-10-30 AR ARP020104114A patent/AR037743A1/es not_active Application Discontinuation
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2004
- 2004-05-28 NO NO20042229A patent/NO20042229L/no unknown
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NO20042229L (no) | 2004-05-28 |
EP1463509A1 (en) | 2004-10-06 |
MXPA04003668A (es) | 2004-07-22 |
US20040259863A1 (en) | 2004-12-23 |
JP2005515975A (ja) | 2005-06-02 |
HUP0401984A3 (en) | 2005-06-28 |
AR037743A1 (es) | 2004-12-01 |
SK1862004A3 (en) | 2004-08-03 |
CA2462525A1 (en) | 2003-05-08 |
WO2003037349A1 (en) | 2003-05-08 |
CN1578665A (zh) | 2005-02-09 |
CZ2004516A3 (cs) | 2004-08-18 |
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